冉冉升起的新星:核酸适配体

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是 Bio-Techne 旗下子公司之一,在生命科学研究领域拥有 30 余年的历史,产品涵盖 3,500 种小分子化合物和 500 种生物多肽,涉及激动剂、抑制剂、神经递质等。Tocris 始终追求卓越品质,以提供最新的产品及创新的工具享誉全球。","nodeType":"3","display":"inline","nodeAttrs":[],"childNodes":[]}]}]}]}]}]}]}]}]}]},"imageUrls":["https://image109.360doc.com/DownloadImg/2021/03/3000/218816013_1_20210330120756771","https://image109.360doc.com/DownloadImg/2021/03/3000/218816013_2_20210330120756912","https://image109.360doc.com/DownloadImg/2021/03/3000/218816013_3_2021033012075737","https://image109.360doc.com/DownloadImg/2021/03/3000/218816013_4_2021033012075799"],"text":"核酸适配体(aptamers),不少人对这一概念还比较陌生,事实上,国内外诸多科学家已聚焦该领域,它的巨大潜力也逐渐被挖掘。核酸适配体是短的单链 DNA 或 RNA 分子,可以与靶标分子进行高选择性和高亲和力的结合。核酸序列具有独特的三维结构,使得核酸适配体倾向于形成螺旋和单链环,有助于目标的选择性。核酸适配体与靶标结合,图片来源:10.1038/mtna.2014.32核酸适配体也被称为「化学抗体」,但与抗体相比有一定的优势:无免疫原性、易于生成、体积小、化学稳定性高。此外,由于它们是化学合成的,便于进行修饰以改善药代动力学、添加荧光基团或光敏基团。核酸适配体用途广泛,如探测细胞表面分子的功能和感知或调节细胞表面的相互作用。核酸适配体是通过指数富集的配体系统进化技术(Systematic Evolution of Ligands by EXponential enrichment,SELEX)筛选分离而得,该技术在 1990 年由 Tuerk 和 Gold 首次提出。这一体外程序是将合成的单链 DNA 和 RNA 文库与靶标分子共孵育,随后用 PCR 分离并扩增目标结合序列,循环重复该过程,直到获得针对特定目标序列的富集文库,最后克隆并测序以识别单个核酸适配体。SELEX 筛选系统示意图,图片来源:doi: 10.3390/biomedicines5030045.这种 SELEX 策略最常应用于蛋白,但也可广泛应用于小分子化合物、活细胞、组织和微生物等靶标。近年来,将整个活细胞作为复杂靶标(称为 cell-SELEX)的研究也备受关注,其优势在于能够在生理条件下选择核酸适配体。因而,核酸适配体在电化学、蛋白质组学、临床医学、药物研发及基因调控等领域具有广阔的应用前景。例如:用于生物成像探针,生物传感器;体外肿瘤细胞检测、体内肿瘤成像和靶向肿瘤治疗;药物开发:作为靶向药物的导向分子,用于疾病的精准医疗。例如首个核酸适配体药物哌加他尼(Pegaptanib);可逆地与靶标分子结合的能力,控制药物的释放;病毒检测及抗病毒治疗:可在不同的实验环境中抵抗多种病毒,包括甲型和乙型流感病毒、呼吸道合胞病毒(RSV)和 SARS 冠状病毒(SARS-CoV)。 核酸适配体的应用,图片来源:10.1038/mtna.2014.32.Tocris® 提供多种高亲和力、荧光标记的核酸适配体,产品不断增加中:Cat. No.产品名称/活性6556Anti-human EGFR aptamer, Janelia Fluor® 646 conjugateHigh affinity anti-human EGFR aptamer conjugated to Janelia Fluor® 6466557Anti-human ErbB2 aptamer, Janelia Fluor® 646 conjugateAnti-human ErbB2 aptamer, Janelia Fluor® 646 conjugate6103CD133-A15, 5'-DY647High affinity fluorescently tagged aptamer for CD133 (AC133 epitope)6104CD133-B19, 5'-DY647High affinity fluorescently tagged aptamer for CD133 (extracellular domain epitope)5609DFHBIMimic of GFP fluorophore for imaging RNA in living cells; activated by binding Spinach2 and Broccoli aptamers5610DFHBI 1TMimic of GFP fluorophore for imaging RNA in living cells; activated by binding Spinach2 and Broccoli aptamers6434DFHOMimic of RFP fluorophore for imaging RNA in living cells; activated by binding Corn aptamers6102Ep23, 5'-DY647High affinity fluorescently tagged aptamer for EpCamTocris® 是 Bio-Techne 旗下子公司之一,在生命科学研究领域拥有 30 余年的历史,产品涵盖 3,500 种小分子化合物和 500 种生物多肽,涉及激动剂、抑制剂、神经递质等。Tocris 始终追求卓越品质,以提供最新的产品及创新的工具享誉全球。"}

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